N-[2-(m-methoxyphenyl)ethyl]-N-ethyl-2-(1-pyrrolidinyl)ethylamine (UMB 116) is a novel antagonist for cocaine-induced effects.

N-[2-(m-methoxyphenyl)ethyl]-N-ethyl-2-(1-pyrrolidinyl)ethylamine (UMB 116) is a novel antagonist for cocaine-induced effects. Research Abstract Details 

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N-[2-(m-methoxyphenyl)ethyl]-N-ethyl-2-(1-pyrrolidinyl)ethylamine (UMB 116) is a novel antagonist for cocaine-induced effects. Abstract Text:

AnTawan Daniels,Erika Ayala,Weibin Chen,Andrew Coop,Rae R Matsumoto,

Previous research has shown that sigma receptors participate in the actions of cocaine in the body. This has led to investigations of the use of novel agents such as BD1008, BD1067 and YZ-011 as cocaine antagonists. In the present study, three novel analogs (UMB115, UMB116, UMB117), representing composites of these earlier compounds, were evaluated in receptor binding and behavioral studies. In the receptor binding studies, the compounds were shown to have high affinity for sigma receptors and much lower affinities for non-sigma sites. For the behavioral experiments, Swiss Webster mice were pre-treated with saline or one of the novel compounds (0.1-10 mg/kg), followed 15 min later by a convulsive (60 mg/kg), lethal (125 mg/kg), or locomotor stimulatory (10 mg/kg) dose of cocaine. The results showed that UMB115, UMB116 and UMB117 significantly (P<0.05) inhibited cocaine-induced convulsions when administered as a pre-treatment to cocaine. Cocaine-induced lethality was significantly attenuated by UMB116 (P<0.05), but not by UMB115 and UMB117. All three compounds significantly (P<0.05) altered the locomotor stimulatory effects of cocaine, with UMB115 and UMB116 exhibiting attenuating actions. Together, the studies suggest UMB116 as a novel cocaine antagonist.

N-[2-(m-methoxyphenyl)ethyl]-N-ethyl-2-(1-pyrrolidinyl)ethylamine (UMB 116) is a novel antagonist for cocaine-induced effects. Publishing Authors By Initials

A Daniels,E Ayala,W Chen,A Coop,RR Matsumoto,

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N-[2-(m-methoxyphenyl)ethyl]-N-ethyl-2-(1-pyrrolidinyl)ethylamine (UMB 116) is a novel antagonist for cocaine-induced effects. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: European journal of pharmacology

VOLUME: 542

Page Numbers: 61-8

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ISSN: 0014-2999

DAY: 5

MONTH: 04

YEAR: 2006

N-[2-(m-methoxyphenyl)ethyl]-N-ethyl-2-(1-pyrrolidinyl)ethylamine (UMB 116) is a novel antagonist for cocaine-induced effects. Information

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LANGUAGE: eng

NlmUniqueID: 1254354

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Grant and Affiliation Information for N-[2-(m-methoxyphenyl)ethyl]-N-ethyl-2-(1-pyrrolidinyl)ethylamine (UMB 116) is a novel antagonist for cocaine-induced effects.

AFFILIATION: Department of Pharmaceutical Sciences, College of Pharmacy, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73190, USA.

Country: Netherlands

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MEDLINETA: Eur J Pharmacol

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